Skin-lightening composition

ABSTRACT

A light colored standardized extract of  Emblica officinalis  consisting essentially of over 40% by weight of Emblicanin A. Emblicanin B, Pedunculagin and Punigluconin, and not more than about 1% by weight of flavonoids, and methods of producing same. Also disclosed are cosmetic or pharmaceutical compositions comprising the standardized extract and methods of using same to lighten or whiten skin.

FIELD OF THE INVENTION

This invention relates to novel skin lightening or whitening or eventoning compositions and methods of administering same for theirpharmaceutical, cosmetic and aesthetic applications.

BACKGROUND OF THE INVENTION

As stated in the scientific literature, the type and amount of melaninsynthesized by the melanocyte and its distribution pattern in thesurrounding keratinocytes determines the actual color of the human skin.Melanin forms through a series of oxidative reaction involving the aminoacid tyrosine in the presence of the enzyme tyrosinase. The first stepis the most critical because the remainder of the reaction sequences canproceed spontaneously at physiological pH. Thus, tyrosinase convertstyrosine to dihydroxyphenylalanine (DOPA) and then to dopaquinone.Subsequently, dopaquinone converted to dopachrome, throughautooxidation, and finally to dihydroxyindole ordihydroxyindole-2-carboxylic acid (DHICA) to form eumelanin (brown-blackpigment). The later reaction occurs in the presence of dopachrometautomerase and DHICA oxidase. In the presence of cysteine orglutathione, dopaquinone is converted to cysteinyl DOPA or glutathioneDOPA. Subsequently, pheomelanin, a yellow-red pigment, is formed.

The color of the skin and its intensity therefore depend an the rate offormation of the melanin, its degree of polymerization, the speed ofexfoliation and the thickness of the horny layer, i.e. the layer thatcontains the most pigment. For a more detailed discussion of thepigmentation pathway, attention is invited to “Skin DepigmentingAgents”, Michael P. Tabibran M.D., (Medicine Journal, Jul. 8, 2001, Vol.2, November 7.)

In general, to reduce cutaneous pigmentation, it is necessary to reducethe rate of formation of the melanin by inhibiting the tyrosinase whileretarding its polymerization and accelerating the exfoliation of thehorny layer.

For purposes of skin lightening or whitening or even toning, topicalapplication of skin lightening or whitening or even toning agent shouldhave a lightening, whitening or even toning effect an the only area tobe treated, produce neither irritation nor post-inflammatory secondarypigmentation, and cause neither a systemic depigmenting effect nor anallergic reaction.

In addition, the skin lightening, whitening or even toning should beeffective for normal cutaneous pigmentation and its excesses: includingbut not limited to lentigo senilis, chloasma, hyperpigmentation afteruse of photosensitizing products, and cicatrical brown spots.

In French patent 2730408 published Aug. 14, 1996, composition areproposed to regulate cutaneous pigmentation, based an extracts of fruitsamong which is Phyllantus emblica (syn.Eniblica offtcirzalis). Thecomposition may be based an a dilute-alcoholic extract obtained from thePhyllantus emblica or an extract obtained, for example by merelypressing the fruit.

Both the extracts obtained by pressing and the extracts obtained byalcoholic maceration may then be concentrated at a moderate temperatureunder reduced pressure, preferably less than 50° C., then optionallybrought to the dry state by freeze-drying or any other method underreduced pressure and at a temperature that is lower than 50° C. so as toavoid degrading the active ingredients of the fruit. In greater detail,examples 3, 6 and 8 of the French patent 2730408 illustrate themanufacture and uses of extracts based an Phyllantus emblica.

In this French patent, however, there is no indication of thecomposition or the chemical nature of the extracts being defined.Conversely, in U.S. Pat. No. 6,124,268, Ghosal, issued Sep. 26, 2000entitled “Natural Oxidant Compositions, Method For Obtaining Same AndCosmetic, Pharmaceutical and Nutritional Formulations Thereof’ there isset forth the chemical temperatures, e.g. 70° C., using a very diluteaqueous or alcoholic-water salt solution, e.g. 0.1 to 5%. By thisextraction process, in the presence of sodium chloride, for example,hydrolysis of the glycocidic enzymes in the plant is prevented and theproduct is protected from microbial infestation.

In the Ghosal patent, the antioxidant blend of the constituents isdescribed under the name of “CAPROS”, with claim 8, for example, of thepatent setting forth the composition as follows:

An antioxidant blend consisting essentially of, by weight, (1) and (2)about 35-55% of the gallic/ellagic acid derivatives of2-keto-glucono-8-lactone; (3) about 4-15% of2,3-di-O-galloyl-4,6-(S)-hexahydroxydiphenoylgluconic acid; (4) about10-20% of 2,3,4,6-bis-(S)-hexahydroxydiphenoyl-D,-glucose; (5) about5-15% of 3′,4′,5,7-tetrahydroxyflavone-3-0-rhamnoglucoside; and (6)about 10-30% of tannoids of gallic/ellagic acid.@

The common names of the enumerated compounds are (1) and (2) EmblicaninA and Emblicanin B, (3) Punigluconin, (4) Pedunculagin and (5) Rutin.There is no mention of its utility as a skin lightening or whitening oreven toning agent has been indicated by Ghosal.

With respect to acceptability of the products of the French and U.S.Patents for the purposes of skin whitening, they have one or moredisadvantages.

An object of the present invention, therefore, is to provide a novelcomposition and method for whitening or lightening or even toning skinfor the above described cosmetic and dermatological indications amongothers.

Upon further study of this application, other objects and advantages ofthe invention will become apparent.

SUMMARY

It has been discovered that a closely related but novel standardizedantioxidant composition based on an extract of Emblica officinalisprovides a more acceptable skin whitening composition and method of use.

The antioxidant composition used in the present invention comprises amodification of the CAPROS composition, comprising a standardizedextract of low molecular weight <<000) hydrolyzable tannins, over 40%,preferably 50-80%. w/w of Emblicanin A, Emblicanin B, Pedunculagin, andPunigluconin with low levels <<O/G, w/w) of total flavonoids whereby theresultant products of the invention can be made into elegant white tooff-white formulations. Such a composition is discussed with greaterspecificity in pages 28-30 of the August 2001 issue of Soap, Perfumeryand Cosmetics, the article having the title Ingredients/Emblica, BearingFrait, by Ratan K. Chaudhuri. In that article there is no mention,however, of any flavonoids much less the maximum acceptable amounts inthe composition.

According to the present invention, the total flavonoids are maintainedat a level which does not impair the desired color, e.g. generally, byweight, less than about 1.0%, preferably less than about 0.8%, and evenmore preferably less than about 0.6%. In comparison, commercialcompetitive products have significantly higher contents of totalflavonoids and exhibit a significantly darker color. Also, the desiredconcentrations of the Rutin species of flavonoids(3′,4′,5′,7′-tetrahydroxyflavone-3-0-rhamnoglucoside) in thestandardized extract are less than 1.0%, less than 0.01%, less than0.001% and less than 0.0001%, with a value of 0.01 to 0.001% beingparticularly preferred. The most preferred concentrations of thecomponents are an a percent by weight basis of the total dried extract:Most Preferred Concentrations Product Identity % by weight Emblicanin A20-35 Emblicanin B 10-20 Pedunculain 15-30 Punigluconin  3-12 TotalFlavonoids <1

The standardized composition may exhibit average percentage deviationsfrom these preferred values of: Product Identity Preferred DeviationMost Preferred Deviation Emblicanin A ±10% ±50%  Emblicanin B +10% ±5%Pedunculagi ±10% ±5% Punigluconin ±10% ±5% Total Flavonoids ±10% ±5%

The antioxidant composition can be obtained by removal of the totalflavonoids by reversed-phase column chromatography or HPLC using asolvent System of acetonitrile, water/phosphoric acid (20/80/1) or othersolvent combinations as they elute faster than the low molecular-weighttannins. Also, by selection of geographical location, the Phyllanthusemblica fruit extract may provide a substantially lower level of thetotal flavonoids (<1.0%). It has been observed that medium-sized fruitscollected from some parts of eastern India, during October-November,alter water extraction and drying, yielded the preferred antioxidantcomposition as a powder with the desired low content of totalflavonoids. Accordingly, by analyzing the total flavonoids content ofextracts and selecting such extracts that contain the desired lowcontent of total flavonoids, it is possible to prepare a standardizedextract.

In the context of the present invention “flavonoids” include a family ofcompounds which exhibit a peak at 350 nm when analyzed by W spectraldata. Examples of flavonoids include but are not limited to flavonoidsand flavones, a species thereof being Rutin as discussed above.

In general, the standardized extract is sold as a powder in packagedform, e.g. in drums, in amounts of generally at least 500 g, withsamples weighing about 50 g. Larger or smaller commercial shipments arealso possible, the oily proviso being that the powder in the package hasbeen analyzed and conforms to the above tabulated specifications. Inorder to obtain the packaged powder with the desired specifications, an.optional process comprises blending different batches of powderedextract, with at least one batch being below specification, but with theblend meeting specifications.

The resultant standardized extract powdery material is then incorporatedin a cosmetically or pharmaceutically acceptable carrier, preferablyhaving a pH of about between 3 to 6.5. The carrier is any conventionalcarrier for topical administration and is preferably employed in aconcentration of about 90% to 99.7%, preferably 95 to 99.5. (In otherwords, the concentration of the antioxidant composition of the presentInvention is generally about 0.3 to 10% by weight, preferably 0.5 to 5%by weight.)

In addition to or included with the above mentioned disorders for whichthis invention can be of use, are without limitation: frecklesreduction, reduction of yellow mass-tone an Asians skins and inhibitionof skin Dischromia related to the aging process, as well as a reductionin redness linked to venous disorders and a reduction in W-inducedpigmentation.

The antioxidant composition and formulation of the present invention canbe optionally mixed with other skin whitening agents, either known priorto the present disclosure as well as those which will be invented in thefuture. For example, the skin whitening products which can be combinedinclude but are not limited to cysteine, 4-thioresorcin,3-aminotyrosine, 5-hydroxy-2-hydroxymethyl-y-pyridone, fomesjaponicusand ganoderma extracts, kojic acid, glabridin, ligorice extract,glycyrrhizinic acid, hydroquinone-β-glucoside, catharanthus roseusextract, proteoglycans, proteinase inhibitors, oligopeptides, betaines,and methyl 4-benzyloxy-2-hydroxybenzoate and4-benzyloxy-2-hydroxybenzoic acid. In addition to skin whiteningactivity, the compositions and formulations of the present Invention areeffective photoprotective agents and can be optionally blended withother photoprotective agents.

As for the optional photoprotective agents, if sunscreens are added,suitable sunscreens include any agent capable of protecting the skinfrom W radiation including, for example, butyl methoxydibenzoylmethane,cinoxate, benzophenone-8, homosalate, menthyl anthranilate, octocrylene,ethyhexyl methoxycinnamate, ethylhexyl salicylate, benzophenone-3,ethylhexyl dimethyl PABA, glyceryl PABA, phenylbenzimidazole sulfonicacid, benzophenone-4, ethyhexyl triazone, diethylhexyl butamidotriazone, bisimidazylate etc.

For the purposes of providing a topical formulation with the activecompound or compounds of the present invention, any of the known topicalexcipients can be used therewith such as mineral oils, emulsifyingagents, preservatives, anti-oxidants, skin penetrants, etc., includingbut not limited to the various topical excipients which are utilized inthe Ghosal patent 6,124,268 and the references discussed above. Thecompositions can be employed as a typical topical compositions employedin the dermatological and cosmetic field, e.g., Lotions, gels,emulsions, sprays, sticks, liposomes, etc.

With respect to the amount of the topical composition which is appliedto the skin, it should be a sufficient amount and for a sufficientperiod of time to ‘visibly whiien the skin. Preferably the topicalcomposition contains’ an amount of 0.3 to 5.0% by weight of theinventive composition in a formulated product and preferably for atleast about once per day for a period of preferably at least about twoweeks.

Without further elaboration, it is believed that one skilled in the artcan, using the preceding description, utilize the present invention toits fällest extent. The following preferred specific embodiments are,therefore, to be construed as merely illustrative, and not Einitative ofthe remainder of the disclosure in any way whatsoever.

In the foregoing and in the following examples, all temperatures are setforth uncorrected in degrees Celsius; and, unless otherwise indicated,all parts and percentages are by weight.

The entire disclosures of all applications, patents and applications,cited above or below is hereby incorporated by reference.

Examples of lotions include but are not limited to the followingformulations: TABLE 1 Moisturizing Lotion with 0.5% Emblica ™ INCI NAME% w/w Phase A-1 Water (demineralized) 59.15 Disodium EDTA 0.05 PropyleneGlycol 5.00 Phase A-2 Xantham Gum 0.20 Phase B PEG-6 stearate,ceteth-20, glyceryl 10.00 stearate, steareth-20, stearic acid StearicAcid 1.00 Hydrogenated castor oil 1.00 Octyldodecyl myristate 8.00Dimethicone 4.00 Phenyltrimethicone 2.00 Sweet Almond oil 3.00 Phase CWater (demineralized) 5.00 Phyllanthus emblica fruit extract 0.50 PhaseD Triethanolamine 0.10 Phase E Phenoxyethanol, Isopropylparaben, 1.00Isobutylparaben, Butylparaben Total 100.00Procedure

Disperse A-2 in A-1 and hegt to 70-75° C. Combine B and heat to 70-75°C. Add B to A while stirring. Homogenize until mixture cools to 60° C.At 30° C. add phase C. Adjust pH with TEA to 5.0-6.0. Add phase E. Mixuntil uniform. TABLE 2 Lotion with 0.5% Emblica ™ INCI NAME % w/w PhaseA Water (demineralized) 66.61 Disodium EDTA 0.10 Propylene Glycol 2.00Sorbitol 2.00 Sodium Lauryl Sulfate 0.15 Phase B Glyceryl stearate 5.00Stearic Acid 1.00 Persea Gratissima (Avocado) oil 15.00 UnsaponifiablesBeeswax 1.50 Phase C Water (demineralized) 5.00 Phyllanthus emblicafruit extract 0.50 Phase D Triethanolamine 0.14 Phase E Propyleneglycol, DMDM Hydantoin, 1.00 Methylparaben Total 100.00Procedure

Combine A and heat to 70-75° C. Combine B and heat to 70-75° C. Add B toA while stirring. Add phase C at 30° C. Adjust pH to 5.0-6.0 with phaseD. Add phase E. Mix until uniform. TABLE 3 Lotion with Emblica ™ (O/W)INCI NAME % w/w Phase A Paraffinum Liquidum (Mineral Oil) 8.00Trilaureth-4 Phosphate 1.50 Polyglyceryl-2 Sesquiisostearate 2.00Isopropyl Palmitate 6.00 Octyl Stearate 5.00 Carbomer 0.40 Phase BGlycerin 3.00 Preservatives q.s. Water (demineralized) 68.60 Phase CWater (demineralized) 5.00 Phyllanthus emblica fruit extract 0.50 PhaseD Triethanolamine q.s. Phase E Total 100.00Procedure

Mix phases A and B separately. Add phase B into A. Add phase C.Neutralize with phase D. Homogenize.

Note

-   pH=6.00

Viscosity 5200 mPa.s (Brookfield RVT, T-B, 10 rpm) TABLE 4 Lotion with1.0% Emblica ™ INCI NAME % w/w Phase A Water (demineralized) 65.97Disodium EDTA 0.10 Propylene Glycol 2.00 Sorbitol 2.00 Sodium LaurylSulfate 0.15 Phase B Glyceryl stearate 5.00 Stearic acid 1.00 PerseaGratissima (Avocado) oil 15.00 Unsaponifiables Beeswax 1.50 Phase CWater (demineralized) 5.00 Phyllanthus emblica fruit extract 1.00 PhaseD Triethanolamine 0.28 Phase E Propylene glycol, DMDM Hydantoin, 1.00Methylparaben Total 100.00Procedure

Combine A and heat to 70-75° C. Combine B and heat to 70-75° C. Add B toA while stirring. Add phase C at 30° C. Adjust pH to 5.0-6.0 with phaseD. Add phase E. Mix until uniform. TABLE 5 Skin Lightening Lotion INCINAME % w/w Phase A-1 Water (demineralized) 55.05 Disodium EDTA 0.05Propylene Glycol 5.00 Phase A-2 Xantham Gum 0.25 Magnesium aluminumstearate 0.40 Phase B Cetearyl alcohol and cetearyl glucoside 7.00Apricot kernel oil 10.00 Octyl stearate 3.00 Dimethicone 6.00 Phase CWater (demineralized) 10.00 Phyllanthus emblica fruit extract 2.00 PhaseD Triethanolamine 0.25 Phase E Phenoxyethanol, Isopropylparaben, 1.00Isobutylparaben, Butylparaben Phase F Fragrance 0.25 Total 100.00Procedure

Disperse A-2 in A-1 and heat to 70-75° C. Combine B and heat to 70-75°C. Add B to A while stirring. Homogenize until mixture cools to 60° C.At 30° C. add phase C. Adjust pH with TEA to 4.0-5.0. Add phase E. AddF. Mix until uniform. TABLE 6 Skin Lightening Lotion INCI NAME % w/wPhase A-1 Water (demineralized) 56.18 Disodium EDTA 0.05 PropyleneGlycol 5.00 Phase A-2 Xantham Gum 0.25 Magnesium aluminum stearate 0.40Phase B Cetearyl alcohol and cetearyl glucoside 7.00 Apricot kernel oil10.00 Octyl stearate 3.00 Dimethicone 6.00 Phase C Water (demineralized)10.00 Phyllanthus emblica fruit extract 1.00 Phase D Triethanolamine0.12 Phase E Phenoxyethanol, Isopropylparaben, 1.00 Isobutylparaben,Butylparaben Phase F Fragrance 0.25 Total 100.00Procedure

Disperse A-2 in A-1 and heat to 70-75° C. Combine B and heat to 70-75°C. Add B to A while stirring. Homogenize until mixture cools to 60° C.

At 30° C. add phase C. Adjust pH with TEA to 4.0-5.0. Add phase E. AddF. Mix until uniform. TABLE 7 Lotion with 0.2% Emblica Formulation # EUS18-87 INCI NAME % w/w Phase A Water (demineralized) 50.73 Na2 EDTA 0.05Propylene Glycol 5.00 Phase B PEG-6 Stearate and Ceteth-20 and 10.00Glyceryl Stearate and Steareth-20 Glyceryl Stearate and PEG-100 Stearate6.00 Stearyl alcohol 3.00 Dimethicone 4.00 Phase C Water (demineralized)10.00 Emblica oficinalis fruit extract 0.20 Phase D Triethanolamine 0.02Phase E Phenoxyethanol, Isopropylparaben, 1.00 Isobutylparaben,Butylparaben Total 100.00Procedure

Combine A and heat to 70-75° C. Combine B and heat to 70-75° C. Add B toA under agitation. Homogenize mixture. Add C at 40° C. Adjust pH to4.0-5.0 with D. Add E. Mix until mixture reaches RT. TABLE 8 Lotion with0.5% Emblica Formulation # EUS 18-89 INCI NAME % w/w Phase A Water(demineralized) 60.39 Na2 EDTA 0.05 Propylene Glycol 5.00 Phase B PEG-6Stearate and Ceteth-20 and 10.00 Glyceryl Stearate and Steareth-20Glyceryl Stearate and PEG-100 Stearate 6.00 Stearyl alcohol 3.00Dimethicone 4.00 Phase C Water (demineralized) 10.00 Emblica oficinalisfruit extract 0.50 Phase D Triethanolamine 0.06 Phase E Phenoxyethanol,Isopropylparaben, 1.00 Isobutylparaben, Butylparaben Total 100.00Procedure

Combine A and heat to 70-75° C. Combine B and heat to 70-75° C. Add B toA under agitation. Homogenize mixture. Add C at 40° C. Adjust pH to4.0-5.0 with D. Add E. Mix until mixture reaches RT.

COMPARISON OF PREFERRED EMBODIMENTS VERSUS COMMERCIAL COMPOSITIONS

In the following tables there are presented representative analyses ofcomponents of Applicants' products versus commercial products, and alsoa table which compares the absorbances of Applicants' product versus thecommercial products. The latter table is important for it demonstratesthat products of the invention have a lighter color and can beformulated into aesthetically superior products than the commercialextracts. As such, the following tables are self-explanatory.

Table I

Percentage Total Flavonoids (% w/w) Present in the Product of PresentInvention vs Commercial Products % Examples Supplier Lot NumberFlavonoids 1 Present Invention CA 0107009 0.93 2 Present Invention CA0107010 0.91 3 Present Invention CA0107011 0.84 4 Present Invention CA0107012 0.88 5 Present Invention 8001 0.46 6 Present Invention KAMJ-5440.68 7 Ayush Herbs, Inc., USA Ay/Amla/00461 7.77 8 Geni, Inc., USA*AML-01 2.75 9 Geni, Inc., USA AME-T1 4.06 10 Geni, Inc., USA AME-T2 3.4111 Rose Color, R-8 1.91 Inc., USA 12 Trippie Crown America, EO-0525 3.02Inc. USA 13 Tripple Crown America, EG-0792 2.7 Inc. USA 14 Tripple CrownAmerica, EO-1584 2.89 Inc. USAMethod of Analysis

Quantification of total flavonoids was done using Rutin as an externalstandard and by calculating % area of peaks.

-   Solvent system: Acetonitrile:Water:Phosphoric acid(20:80:1)-   Flow rate: 0.8 ml/mim-   Column: Merck-Hilbar® Prepacked Column RT 250-4, LiChrosorb® RP-18

Detection: UV detector at 350 nm TABLE II Percentage Total LowMolecular-Weight (<1.000) Tannins Present in the Product of PresentInvention vs. Commercial Products % Low Molecular- WeightTanninsSupplier Lot Number in the Product Present Invention CA 0012006 75.48Present Invention CA 0107010 72.94 Present Invention CA0106007 75.48Present Invention CA0008002 67.53 Present Invention 4001 67.73 A ushHerbs, Inc., USA A/Amis/00461 9.03 Geni, Inc., USA* AML-01 44.17 Geni,Inc., USA AME-T1 17.20 Geni, Inc., USA AME-T2 18.00 Rose Color, Inc.,USA R-8 23.40 Tripple Crown America, EO-0525 29.60 Inc. USA TrippleCrown America, EO-0792 28.91 Inc. USA Tripple Crown America, EO-158429.49 Inc. USA

TABLE III Percentage Low Molecular-Weight (<1.000) Tannins Present inthe Product of Present Invention vs. Commercial Products Product LotEmblicanin Emblicanin Punigiu- Number A B conin Pedunculagin CA 001.200622.47 17.11 10.16 25.73 CA 0107010 26.59 14.86 10.32 21.17 CA010600727.95 16.36 8.20 24.81 GA0008002 21.84 16.29 7.61 21.79 4001 29.32 14.914.79 18.72 Ay/Amia/ 4.55 2.30 1.92 0.27 00461 AML-01 * 18.10 12.14 9.434.50 AME-T1 8.27 2.93 3.11 2.88 AME-T2 8.58 3.07 3.23 3.12 R-8 9.79 7.945.31 0.36 EO-0525 9.94 9.25 9.49 0.92 EO-0792 9.21 9.78 8.83 1.09EO-1584 10.35 9.29 8.78 1.08* This product is very dark and difficult to formulate with due to alarge amount of waterinsoluble polymeric tannins. The relatively lightcolored products of this invention have a relatively small amount ofsuch water-insoluble polymeric tannins and as such, they do notmaterially affect the advantages of the invention, namely the desiredlight color and relative ease of formulations.

TABLE IV Comparative Color Profile of Products Obtained from the PresentInvention vs Commercially Available Products Absorbance (opticaldensity) at different wavelengths No. Supplier Lot Number 350 410 470530 590 650 1 Present Invention CA 0107009 .621 .152 .037 .033 .012 .0042 Present Invention CA 0107010 .644 .153 .036 .028 .020 .004 3 PresentInvention CA 0107011 .604 .140 .036 .020 .004 .004 4 Present InventionCA 0107012 .530 .124 .019 .012 .005 .002 5 Present Invention CA 0008002.595 .196 .063 .035 .021 .021 6 Present Invention CA 0012006 .558 .180.048 .024 .012 .006 7 Ayush Herbs, Inc., USA Ay/Amla/00461 >2.25 1.43.692 .396 .285 .248 8 Geni, Inc., USA AML-01 >2.25 1.08 .600 .375 .250.175 9 Geni, Inc., USA AME-T1 >2.25 1.27 .540 .311 .195 .150 10 Geni,Inc., USA AME-T2 >2.25 1.29 .680 .448 .332 .274 11 Rose Color, Inc., USAR-8 >2.25 .999 .148 .074 .351 .036 12 Tripple Crown America,EO-0525 >2.25 1.15 .672 .474 .364 .276 Inc. USA 13 Tripple CrownAmerica, EO-0792 >2.25 1.73 1.05 .776 .606 .504 Inc. USA 14 TrippleCrown America, EO-1584 >2.25 1.33 :800 .575 .475 .35 Inc. USAMethod of Analysis

Test compounds (0.5 g) were weighed and dissolved in distilled water(100 ml) by sonicating for 10 min to give a final concentration of 0.5%(w/v). The resulting solution was filtered and the absorbance wasrecorded between X 350 to 650 nm, against distilled water in a DU-64Spectrophotometer.

Results

Six samples (#1-6) of the Present invention clearly exhibit much lessabsorbance values at the six different wavelengths (350-650 nm)determined in the study. All other samples (#7-14) exhibit much higherabsorbance values at the respective wavelengths studied than any othersamples of the Present invention.

Conclusion

The study clearly indicates the color intensity of competitive materialsis five to over ten times higher in the wavelengths studied. Formulatedproducts containing these materials is found to. De much darker(unacceptable to consumers and have limited shelf life) color even atlow concentrations (−0.1%) whereas formulated products prepared usingthe material of the present invention have much better color at anylevel (˜0.1 to 3% level).

Accordingly, preferred subgeneric aspects of this invention include butare not limited to standardized extracts having an absorbance (opticaldensity) of 0.8 maximum in the UV region at wavelength 350 nm and/or amaximum of 0.3 in the UV region at wavelength 410 nm and/or a maximum of0.1 nm in the UV region at wavelength 470 nm and/or a 0.08 maximum inthe UV region at wavelength 530 nm, and/or a maximum of 0.09 in the UVregion at wavelengths 590 nm and/or a maximum of 0.02 in the UV regionat wavelength 650 nm. Thus, comprehensive embodiments of standardizedextracts as related to absorbances are those standardized extractshaving 2, 3, 4, 5 or 6 of the above absorbances, with the mostcomprehensive having in the UV region a maximum optical density of 0.8at wavelength 350 nm, a maximum optical density of 0.3 at wavelength 410nm, a maximum optical density of 0.1 at wavelength 470 nm, a maximumoptical density of 0.08 at wavelength 530 nm, a maximum optical densityof 0.09 at wavelength 590 nm and a maximum optical density of 0.02 atwavelength 650 nm.

Clinical Example

Thirteen Hispanic and thirteen Asian human volunteers were treated witha test formulation tabulated an the following page entitled “FormulationUsed For Clinical Testing (EMBLICA IV)”.

The test formulation was applied to both the right and left upper armsof the volunteers at a rate of 0.05 ml twice daily for 12 weeks. Theresults were represented using the individual typology angle (COLIPA SPFtest method); measured by chromometric measurement. TABLE 9 FORMULATIONUSED FOR CLINICAL TESTING (EMBLICA) ® Formulation #EUS 17-99 (2%Emblica) INCI NAME % w/w 1.75 kg Phase A Water (demineralized) 58.701027.25 Na2 EDTA 0.05 0.88 Propylene Glycol 5.00 87.50 Phase B PEG-6Stearate and Ceteth-20 and 10.00 175.00 Glyceryl stearate andSteareth-20 Glyceryl stearate and PEG-100 Stearate 6.00 105.00 Stearylalcohol 3.00 52.50 Dimethicone 4.00 70.00 Phase C Water (demineralized)10.00 175.00 Phyllanthus emblica fruit extract 2.00 35.00 Phase DTriethanolamine 0.25 4.38 Phase E Phenoxyethanol and Isopropylparabenand 1.00 17.50 Isobutylparaben and Butylparaben Total 100.00 1750.00

The preceding examples can be repeated with similar success bysubstituting the generically or specifically described reactants and/oroperating conditions of this invention for those used in the precedingexamples.

The entire disclosure of all applications, patents and publications,cited above or below, are hereby incorporated by reference.

From—the foregoing description, one skilled in the art can easilyascertain the essential characteristics of this invention and, withoutdeparting from the spirit and scope thereof, can make various changesand modifications of the invention to adapt it to various usages andconditions.

1. A light colored standardized extract of Emblica officinalisconsisting essentially of over 40% by weight of Emblicanin A. EmblicaninB, Pedunculagin and Punigluconin, and not more than about 1% by weightof flavonoids.
 2. A standardized extract according to claim 1 consistingessentially of by weight 50-80% of Emblican A, Emblican B, Pedunculaginand Punigluconin.
 3. A standardized extract according to claim 1consisting essentially of by weight: 20-35% Emblicanin A, 10-20%Emblicanin B, 15-30% Pedunculagin and 3-12% Punigluconin.
 4. Astandardized extract according to claim 1 packaged in powder form.
 5. Astandardized extract according to claim 3 packaged in powder form.
 6. Astandardized extract according to claim 4 wherein the powder weighs atleast 500 g.
 7. A standardized extract according to claim 5 wherein thepowder weighs at least 500 g.
 8. A method of producing the standardizedextract of claim 6 comprising selecting at least one extract containingnot more than 1% by weight of flavonoids and packaging said at least oneextract in powder form.
 9. A method according to claim 8 furthercomprising prior to said selecting, analyzing said extract to determinethe content of flavonoids.
 10. A composition comprising a standardizedextract according to claim 1 and a cosmetically or pharmaceuticallyacceptable carrier.
 11. A composition according to claim 10 wherein thecontent of said standardized extract is about 90-99.7% by weight.
 12. Acomposition according to claim 10 further comprising a skin-whiteningagent different from said standardized extract.
 13. A compositionaccording to claim 10 further comprising a photoprotective agentdifferent from said standardized extract.
 14. A method of lightening orwhitening or even toning skin color comprising topically administering acomposition according to claim 11 to skin in a sufficient amount and fora sufficient amount of time to visibly whiten or lighten or even toningthe skin.
 15. A standardized extract according to claim 1 wherein thecontent of Rutin is less than 0.01% by weight.
 16. A standardizedextract according to claim 2 wherein the content of Rutin is less than0.01% by weight of Rutin.
 17. A standardized extract according to claim3 wherein the content of Rutin is less than 0.01% by weight of Rutin.18. A composition comprising a standardized extract according to claim15 and a cosmetically or pharmaceutically acceptable carrier.
 19. Acomposition comprising a standardized extract according to claim 16 anda cosmetically or pharmaceutically acceptable carrier.
 20. A compositioncomprising a standardized extract according to claim 17 and acosmetically or pharmaceutically acceptable carrier.
 21. A standardizedextract according to claim 1 having an absorbance (optical density) of0.8 Maximum in the UV region at wavelength 350 nm.
 22. A standardizedextract according to claim 1 having an absorbance (optical density) of0.3 maximum in the UV region at wavelength 410 nm.
 23. A standardizedextract according to claim 1 having an absorbance (optical density) of0.1 maximum in the W region at wavelength 470 nm.
 24. A standardizedextract according to claim 1 having an absorbance (optical density) of0.08 maximum in the UV region at wavelength 530 nm.
 25. A standardizedextract according to claim 1 having an absorbance (optical density) of0.09 maximum in the UV region at wavelength 590 nm.
 26. A standardizedextract according to claim 1 having an absorbance (optical density) of0.02 maximum in the UV region at wavelength 650 nm.
 27. A standardizedextract according to claim 1 having maximum absorbances (opticaldensity) in the UV region of 0.8 at wavelength 410 nm, 0.1 at wavelength470 nm, 0.08 at wavelength 530 nm, 0.09 at wavelength 590 nm, and 0.02at wavelength 650 nm.
 28. A method of lightening or whitening or eventoning skin color according to claim 14, said composition furthercontaining a pharmaceutically or cosmetically acceptable carrier.
 29. Amethod of lightening or whitening or even toning skin color according toclaim 14, said composition further containing one or more sunscreenagents different from said standardized extract.
 30. A method oflightening or whitening or even toning skin color according to claim 14,said composition further containing one or more antioxidants differentfrom said standardized extract.
 31. A method of lightening or whiteningor even toning skin color according to claim 14, comprising one or moreantioxidants and sunscreen agents different from said standardizedextract.
 32. A method of lightening or whitening or even toning skincolor according to claim 14, comprising one or more skin lightening orwhitening or toning agents different from said standardized extract.